(rel)-MC180295 (Synonyms: (rel)-MC180295) |
| カタログ番号GC34124 |
(rel)-MC180295 ((rel)-(rel)-MC180295) は、強力かつ選択的な CDK9-サイクリン T1 阻害剤であり、IC50 は 5 nM であり、他の CDK よりも CDK9 に対して少なくとも 22 倍選択的です。 (rel)-MC180295 は GSK-3α も阻害します。およびGSK-3β。 (rel)-MC180295 ((rel)-(rel)-MC180295) には強力な抗腫瘍効果があります。
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Cas No.: 2237942-08-2
Sample solution is provided at 25 µL, 10mM.
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(rel)-MC180295 is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. (rel)-MC180295 also inhibits GSK-3α and GSK-3β. (rel)-MC180295 has potent anti-tumor effect[1].
(rel)-MC180295 (MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs, such as CDK1-Cyclin B (IC50, 138 nM), CDK2-Cyclin A (IC50, 233 nM), CDK2-Cyclin E (IC50, 367 nM), CDK3-Cyclin E (IC50, 399 nM), CDK4-Cyclin D (IC50, 112 nM), CDK5-P35 (IC50, 159 nM), CDK5-P25 (IC50, 186 nM), CDK6-Cyclin D3 (IC50, 712 nM), and CDK7-CycH/MAT1 (IC50, 555 nM). (rel)-MC180295 also inhibits GSK-3α and GSK-3β[1].(rel)-MC180295 (500 nM) reactivates epigenetically silenced genes by targeting CDK9 without affecting DNA methylation[1].(rel)-MC180295 (0.1 μM) inhibits the proliferation in cancer cells[1].
(rel)-MC180295 (MC180295; 20 mg/kg, i.p., qod) inhibits significant anti-tumor activity in mice bearing SW48 cells, shows no inhibitory activity against human T cell growth in vivo[1].
[1]. Zhang H, et al. Targeting CDK9 Reactivates Epigenetically Silenced Genes in Cancer. Cell. 2018 Nov 15;175(5):1244-1258.e26.
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